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GW779439X

CAS No. : 551919-98-3

MCE 站：GW779439X

产品活性：GW779439X，吡唑并吡啶类化合物，是一种金黄色葡萄球菌 PASTA 激酶 Stk1 抑制剂。GW779439X 增强 β-内酰胺类抗生素对各种 MRSA 和 MSSA 的分离株，有的甚至跨越了从耐药到敏感的断点。GW779439X 是一种 AURKA 抑制剂，可通过 caspases 3/7 诱导细胞凋亡 (apoptosis)。

研究领域：Anti-infection  |  Epigenetics  |  Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：Bacterial  |  Aurora Kinase  |  Apoptosis

In Vitro: GW779439X (2 μM) biochemically inhibits Stk1. GW779439X (5 μM) potentiates ceftaroline activity against a ceftaroline-resistant MRSA strain. GW779439X is able to potentiate the activity of oxacillin against various S. aureus isolates, including both MRSA ａnd MSSA isolates, but the potentiation is clearly strongest in PBP2A-containing strains.
GW779439X has growth inhibition effects on the AGP-01 cell line (IC₅₀= 0.57 μM). GW779439X (1μM) significantly blockS the cell cycle at the G0/G1 phase ａnd sub-G1 phase. GW779439X (1μM; 72 hours; AGP-01 cells) significantly decreases expression levels of genes involved in proliferation progression (c-MYC, NRAS, ａnd CDC25A) ａnd increases expression levels of genes involved in cell cycle blocking (CDKN1A ａnd TP53).

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